Abstract
Based on the scaffold of the pharmacologically selective thyromimetic 2b, structurally a close analog to KB-141 ( 2a), a number of novel N-acylated-α-amino acid derivatives were synthesized and tested in a TR radioligand binding assay as well as in a reporter cell assay. On the basis of TRβ 1-isoform selectivity and affinity, as well as affinity to the reporter cell assay, 3d was selected for further studies in the cholesterol-fed rat model. In this model 3d revealed an improved therapeutic window between cholesterol and TSH lowering but decreased margins versus tachycardia compared with 2a.
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